Telmisartan (Micardis) is an angiotensin II receptor antagonist (ARB) used in the management of hypertension. In addition to blocking the Renin-Angiotensin System (RAS), telmisartan acts as a selective modulator of Peroxisome proliferator-activated receptor gamma (PPAR-γ), a central regulator of insulin and glucose metabolism. Telmisartan has binding affinity 3000 times greater for AT1 than AT2 receptors. Telmisartan also has the longest half life (24 hrs) of all angiotensin II type 1 receptor antagonists.
| Molecular Weight | 514.62 |
| Formula | C33H30N4O2 |
| CAS Number | 144701-48-4 |
| Form | Solid |
| Solubility (25°C) | DMSO 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[5] Yan Wang, et al. Telmisartan Improves Insulin Resistance: A Meta-Analysis
| Related Angiotensin Receptor Products |
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(Sar1,Ile4,8)-Angiotensin II is a functionally selective angiotensin II type 1 receptor (AT1R) agonist. |
| TRV055
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| Alamandine
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| (Sar1)-Angiotensin II
(Sar1)-Angiotensin II, an analogue of Angiotensin II, is a specific agonist of angiotensin AT1 receptor. |
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